Medical Physics Research Today is a free monthly online journal that collates and summarizes the latest research about Medical Physics, including details on medicine, radiotherapy, biomechanics, medical imaging.

Quinazoline derivatives as MC-I inhibitors: evaluation of myocardial uptake using Positron Emission Tomography in rat and non-human primate.

Purohit A, Benetti R, Hayes M, Guaraldi M, Kagan M, Yalamanchilli P, Su F, Azure M, Mistry M, Yu M, Robinson S, Dischino DD, Casebier D

Bristol-Myers Squibb Medical Imaging, N Billerica, MA 01860, USA. ajay.purohit@bms.com

Several quinazoline derivatives were made as mitochondrial complex 1 inhibitors. Compound 4 showed an IC(50) of 11.3 nM and was the most potent compound of this series. The (18)F analog of 4, [(18)F] 4, was injected in the rat and showed high and rapid heart uptake, fast liver clearance, and low blood uptake. Images obtained using a microPET showed clear delineation of the myocardium in normal rats and perfusion deficit in ischemic rats. In the non-human primate, [(18)F] 4 showed rapid uptake and clearance from the myocardium and high liver uptake.

Published 7 August 2007 in Bioorg Med Chem Lett, 17(17): 4882-5.
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